ArticleAntimicrobial agents and chemotherapy2009
CS-8958, a prodrug of the novel neuraminidase inhibitor R-125489, demonstrates a favorable long-retention profile in the mouse respiratory tract.
Article in Antimicrobial agents and chemotherapy, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 75 citations in OpenAlex.
- Long-acting neuraminidase inhibitor laninamivir octanoate (CS-8958) versus oseltamivir as treatment for children with influenza virus infection.Antimicrobial agents and chemotherapy · 2010Trial
- Pharmacologic background and clinical issue of anti-influenza drugs.Fukushima journal of medical science · 2025Review
- Antiviral Approaches against Influenza Virus.Clinical microbiology reviews · 2023Review
- Treatment of respiratory viral infections through inhalation therapeutics: Challenges and opportunities.Pulmonary pharmacology & therapeutics · 2022Review
- Antivirals Targeting the Neuraminidase.Cold Spring Harbor perspectives in medicine · 2022Review
- Influenza: overview on prevention and therapy.Australian prescriber · 2019Review
- Re-understanding anti-influenza strategy: attach equal importance to antiviral and anti-inflammatory therapies.Journal of thoracic disease · 2018Review
- Intrapulmonary Pharmacokinetics of Laninamivir, a Neuraminidase Inhibitor, after a Single Nebulized Administration of Laninamivir Octanoate in Healthy Japanese Subjects.Antimicrobial agents and chemotherapy · 2018Article
- Using the Ferret as an Animal Model for Investigating Influenza Antiviral Effectiveness.Frontiers in microbiology · 2016Review
- New small-molecule drug design strategies for fighting resistant influenza A.Acta pharmaceutica Sinica. B · 2015Review
- Clinical pharmacokinetics of inhaled antimicrobials.Clinical pharmacokinetics · 2015Review
- Antiviral strategies against influenza virus: towards new therapeutic approaches.Cellular and molecular life sciences : CMLS · 2014Review
- Peramivir and laninamivir susceptibility of circulating influenza A and B viruses.Influenza and other respiratory viruses · 2014Article
- Zanamivir conjugated to poly-L-glutamine is much more active against influenza viruses in mice and ferrets than the drug itself.Pharmaceutical research · 2014Article
- Therapeutics against influenza.Current topics in microbiology and immunology · 2013Review
- Development of oseltamivir phosphonate congeners as anti-influenza agents.Journal of medicinal chemistry · 2012Article
- Intrapulmonary distribution and pharmacokinetics of laninamivir, a neuraminidase inhibitor, after a single inhaled administration of its prodrug, laninamivir octanoate, in healthy volunteers.Antimicrobial agents and chemotherapy · 2012Article
- Article
- Attaching zanamivir to a polymer markedly enhances its activity against drug-resistant strains of influenza a virus.Journal of pharmaceutical sciences · 2011Article
- Drugs in development for influenza.Drugs · 2010Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
CS-8958 is a prodrug of the pharmacologically active form R-125489, a selective neuraminidase inhibitor, and has long-acting anti-influenza virus activity in vivo. In this study, the tissue distribution profiles after a single intranasal administration of CS-8958 (0.5 micromol/kg of body weight) to mice were investigated, focusing especially on the retention of CS-8958 in the respiratory tract by comparing it with R-125489 and a marketed drug, zanamivir. After administration of [(14)C]CS-8958, radioactivity was retained in the respiratory tract over long periods. At 24 h postdose, the radioactivity concentrations after administration of [(14)C]CS-8958 were approximately 10-fold higher in both the trachea and the lung than those of [(14)C]R-125489 and [(14)C]zanamivir. The [(14)C]CS-8958-derived radioactivity present in these two tissues consisted both of unchanged CS-8958 and of R-125489 at 1 h postdose, while only R-125489, and no other metabolites, was detected at 24 h postdose. After administration of unlabeled CS-8958, CS-8958 was rapidly eliminated from the lungs, whereas the lung R-125489 concentration reached a maximum at 3 h postdose and gradually declined, with an elimination half-life of 41.4 h. The conversion of CS-8958 to R-125489 was observed in mouse trachea and lung S9 fractions and was inhibited by esterase inhibitors, such as diisopropylfluorophosphate and bis-p-nitrophenylphosphate. These results demonstrated that CS-8958 administered intranasally to mice was efficiently converted to R-125489 by a hydrolase(s) such as carboxylesterase, and then R-125489 was slowly eliminated from the respiratory tract. These data support the finding that CS-8958 has potential as a long-acting neuraminidase inhibitor, leading to significant efficacy as an anti-influenza drug by a single treatment.
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